Pharmacological Advancements of PRC2 in Cancer Therapy: A Narrative Review DOI Creative Commons

Michael S. Wang,

Jonathan H. Sussman,

Jun-Jun Xu

и другие.

Life, Год журнала: 2024, Номер 14(12), С. 1645 - 1645

Опубликована: Дек. 11, 2024

Polycomb repressive complex 2 (PRC2) is known to regulate gene expression and chromatin structure as it methylates H3K27, resulting in silencing. Studies have shown that PRC2 has dual functions oncogenesis allow function both an oncogene a tumor suppressor. Because of this, nuanced strategies are necessary promote or inhibit activity therapeutically. Given the therapeutic vulnerabilities associated risks oncological applications, structured literature review on was conducted showcase similar cofactor competitor inhibitors PRC2. Key such Tazemetostat, GSK126, Valemetostat, UNC1999 promise for clinical use within various studies. Tazemetostat GSK126 highly selective wild-type lymphoma-associated EZH2 mutants. Valemetostat orally bioavailable SAM-competitive EZH1 EZH2, giving them greater efficacy against potential drug resistance. The development other inhibitors, particularly targeting EED SUZ12 subunit, also being explored with drugs like 226. This aims bridge gaps current provide unified perspective promising agents treatment lymphomas solid tumors.

Язык: Английский

Pharmacological Advancements of PRC2 in Cancer Therapy: A Narrative Review DOI Creative Commons

Michael S. Wang,

Jonathan H. Sussman,

Jun-Jun Xu

и другие.

Life, Год журнала: 2024, Номер 14(12), С. 1645 - 1645

Опубликована: Дек. 11, 2024

Polycomb repressive complex 2 (PRC2) is known to regulate gene expression and chromatin structure as it methylates H3K27, resulting in silencing. Studies have shown that PRC2 has dual functions oncogenesis allow function both an oncogene a tumor suppressor. Because of this, nuanced strategies are necessary promote or inhibit activity therapeutically. Given the therapeutic vulnerabilities associated risks oncological applications, structured literature review on was conducted showcase similar cofactor competitor inhibitors PRC2. Key such Tazemetostat, GSK126, Valemetostat, UNC1999 promise for clinical use within various studies. Tazemetostat GSK126 highly selective wild-type lymphoma-associated EZH2 mutants. Valemetostat orally bioavailable SAM-competitive EZH1 EZH2, giving them greater efficacy against potential drug resistance. The development other inhibitors, particularly targeting EED SUZ12 subunit, also being explored with drugs like 226. This aims bridge gaps current provide unified perspective promising agents treatment lymphomas solid tumors.

Язык: Английский

Процитировано

0